Revision Year: 2020 Publisher: Merck Serono (Ireland) Limited, 4045 Kingswood Road, Citywest Business Campus, Dublin 24, Ireland
Pharmacotherapeutic group: β-blocking agents, selective (C07AB07)
Bisoprolol is a potent, highly β1-selective adrenoreceptor blocking agent devoid of intrinsic sympathomimetic activity and without relevant membrane stabilising activity.
As with other β1-blocking agents, the mode of action in hypertension is not clear but it is known that bisoprolol markedly depresses plasma renin activity.
In patients with angina, the blockade of β1-receptors reduces heart action and thus reduces oxygen demand. Hence bisoprolol is effective in eliminating or reducing the symptoms.
Bisoprolol is absorbed almost completely from the gastrointestinal tract. Together with the very small first pass effect in the liver, this results in a high bioavailability of approximately 90%. The drug is cleared equally by the liver and kidney.
The plasma elimination half-life (10-12 hours) provides 24 hours efficacy following a once daily dosage. About 95% of the drug substance is excreted through the kidney, half of this is as unchanged bisoprolol. There are no active metabolites in man.
Not applicable.
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